Novel, highly potent and in vivo active inhibitor of GABA transporter subtype 1 with anticonvulsant, anxiolytic, antidepressant and antinociceptive properties

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• 作者：Kinga Sałat^a ; ^{salat.kinga@gmail.com} ; Adrian Podkowa^a ; Natalia Malikowska^a ; Felix Kern^b ; J&ouml ; rg Pabel^b ; Ewelina Wojcieszak^a ; Katarzyna Kulig^c ; ¹ ; Klaus T. Wanner^b ; Beata Strach^d ; Elżbieta Wyska^d
• 关键词：GABA transporter-1 inhibitors ; DDPM-2571 ; Tiagabine ; Mouse models of seizures ; Anxiety ; Depression ; Pain and amnesia ; Brain exposure
• 刊名：Neuropharmacology
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：113
• 期：part_PA
• 页码：331-342
• 全文大小：1423 K
• 卷排序：113

文摘

DDPM-2571, a guvacine analogue, is a novel, potent inhibitor of GABA transporter GAT1. It has prominent anticonvulsant properties in chemically-induced seizures in mice. It demonstrates anxiolytic-like and antidepressant-like properties in vivo. DDPM-2571 has antinociceptive activity in acute and tonic pain models in mice. These pharmacological activities are observed at doses lower than those of tiagabine.